Abstract
Background
Phytoestrogens are natural compounds known as natural selective estrogen receptor modulators used as alternatives against estrogen-dependent cancers. This study aims to evaluate the antiestrogenic effects of Anthonotha macrophylla, a plant used to treat cancer in Cameroon.
Methods
The estrogenic/antiestrogenic activities of A. macrophylla aqueous extract were evaluated in vitro using MCF-7 cell proliferation assay. Moreover, a classical uterotrophic test was carried out to evaluate the antiestrogenic effects of A. macrophylla in rats. Changes in the uterus, vagina, and mammary glands were used as endpoints of estrogenicity.
Results
Anthonotha macrophylla induced antiestrogenic effects in vitro at all the tested concentrations by inhibiting estradiol-induced MCF-7 cell proliferation (p < 0.001). In vivo, a coadministration of estradiol with A. macrophylla extract led to the decrease of uterine [150 (p < 0.05) and 300 (p < 0.01) mg/kg body weight (BW)] and vaginal [75 (p < 0.01) and 300 (p < 0.05) mg/kg BW] epithelial thickness. In addition, a reduction in the mammary gland acini lumen’s diameter was also observed at 75 and 150 mg/kg. Gas chromatography-time-of-flight-mass spectrometry analysis showed that phenolic acid derivatives are present in A. macrophylla extract, which are well known to be endowed with estrogenic/antiestrogenic properties. The LD50 of A. macrophylla was estimated to be less than 2000 mg/kg.
Conclusions
Anthonotha macrophylla aqueous extract has antiestrogenic properties. This could promote more studies to explore its ability to prevent estrogen-dependent cancers.
Acknowledgments
The authors would like to kindly thank Professor Tânia Beatriz Creczynski-Pasa (Federal University of Santa Catarina) for her collaboration. Dr. Stéphane Zingue was a CNPq-TWAS fellow (grant no. 190741/2015-5). The authors would also like to thank the Alexander von Humboldt Foundation for the material support offered to Dieudonné Njamen.
Author contributions: All authors have accepted responsibility for the entire content of this manuscript and approved its submission.
Research funding: None declared.
Competing interests: The authors declare that there are no conflicts of interest regarding the publication of this paper.
Data availability statement: The data used to support the findings of this study are included within the article.
Ethical approval: All the experiments were carried out in strict accordance with the principles and procedures of the European Union concerning the care of animals (EEC Council 86/609) adopted by the National Institutional Ethics Committee of Cameroon, Ministry of Scientific Research and of Technological Innovation (Reg. No. FWA-IRD 0001954).
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